Development and validation an LC-MS/MS method to quantify (+)-borneol in rat plasma: Application to a pharmacokinetic...

Area of Science:

• Pharmacology
• Analytical Chemistry

Background:

• (+)-Borneol, a bicyclic monoterpene, exhibits anti-inflammatory, antioxidant, and GABA receptor-enhancing properties.
• It enhances blood-brain barrier permeability, potentially improving central nervous system (CNS) drug efficacy.

Purpose of the Study:

• To develop and validate a selective liquid chromatography-tandem mass spectrometry (LC-MS/MS) method for quantifying (+)-borneol in rat plasma.
• To evaluate the pharmacokinetics of (+)-borneol following intravenous, oral, and sublingual administration in rats.

Main Methods:

• A rapid LC-MS/MS method using verapamil as an internal standard was established for (+)-borneol analysis in deproteinized rat plasma.
• Positive atmospheric pressure chemical ionization and multiple reaction monitoring (MRM) were employed for sensitive detection.
• The method was fully validated for selectivity, lower limit of quantification (10.0 ng/mL), accuracy, and precision.

Main Results:

• The validated LC-MS/MS method demonstrated excellent selectivity, accuracy, and precision for (+)-borneol quantification.
• Pharmacokinetic studies revealed extremely low oral bioavailability of (+)-borneol in rats.
• Sublingual administration resulted in rapid absorption and favorable bioavailability, outperforming oral delivery.

Conclusions:

• The developed LC-MS/MS assay is suitable for pharmacokinetic studies of (+)-borneol.
• (+)-Borneol exhibits poor oral absorption, but sublingual administration presents a promising alternative for achieving therapeutic concentrations in the CNS.